Acorns gramineus soland is first recorded in the “Shen Nong's Herbal Classic” as top grade and is derived from the dried rhizome of araceae perennial herb, Acorus tatarinowii schott. Acorns gramineus soland has warm property, pungent and bitter taste and aromatic odor, and can entry the heart and stomach meridian. Acorns gramineus soland has aromatic smell, pungent taste and warm property, can remove dampness to restore normal functioning of the stomach and dissipate phlegm for resuscitation, and has the effect of promoting the intelligence and tranquilizing the mind, and thus is commonly used for treatment of stroke, phlegm syncope epilepsy, coma, forgetfulness and so on. The main chemical composition comprises volatile oil mainly containing β-asarone, α-asarone and the like, amino acids and sugars, etc. Modern pharmacological studies suggest that Acorus gramineus soland has anti-dementia, nerve cell protection, anti-mutation, antiepileptic effects and so on.
Polygala tenuifolia is first recorded in the “Shen Nong's Herbal Classic” as top grade and derived from the dried root of polygalaceae polygala tenuifalia Willd. or polygala sibirica L. Polygala tenuifolia has bitter and pungent taste and warm property, and has the effect of promoting the intelligence and tranquilizing the mind, as well as eliminating phlegm and diminishing swelling. The chemical composition of polygala tenuifolia mainly comprises triterpenoid saponins, sugar esters and xanthones, and also contains a small amount of alkaloids, coumarin, lignin and so on. Studies have shown that Polygala tenuifolia has good activity in dementia resisting, brain protection, sedation, convulsion resisting, depression resisting, expectorant and antitussive, cardiovascular and cerebrovascular protection, etc.
Wang Shasha et al. found, in the blood and bile of rats intragastrically administrated with extract of Polygala tenuifolia, active substances 3,4,5-trimethoxycinnamic acid (TMCA), methyl 3,4,5-trimethoxycinnamic acid (M-TMCA) and p-methoxycinnamic acid (PMCA) which can prolong the time of pentobarbital sodium-induced sleep in mice, suggesting the water extract of Polygala tenuifolia contains natural prodrugs of TMCA (WANG S. S. WaKan Iyakugaku Zasshi, 1995, 12(2), 102).
LING Yangzhi et al. performed structural combination of TMCA and obtaind 3,4,5-trimethoxy cinnamamide compounds, which have good anticonvulsant activity (LING Yangzhi, Pharmaceutical Industry, 1987, 18 (2): 56).
Based on the good pharmacological activity of TMCA from Polygala tenuifolia and α-asarone from Acorns gramineus soland in calming, mind tranquillizing, convulsion resisting and nerve cell protection, we designed 3,4,5-trimethoxycinnamate α-Asaronol ester and a series of ester derivatives of α-Asaronol by structural and pharmacophore combination, hoping to obtain new chemical drugs with more effectiveness in senile dementia resisting, brain protection, calming, convulsion resisting, depression resisting and the like.